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    Process for the preparation of pyridopyrimidones
    6.
    发明授权
    Process for the preparation of pyridopyrimidones 有权
    吡啶并嘧啶酮的制备方法

    公开(公告)号：US07119199B2

    公开(公告)日：2006-10-10

    申请号：US11029139

    申请日：2004-12-31

    Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

    Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

    IPC: C07D239/91 ,  C07D471/04

    CPC classification number: C07D239/91 ,  C07D471/04

    Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

    Abstract translation: 本发明涉及一种制备下式的吡啶并吡啶酮的方法，其中X是N或CH，R是芳基，杂芳基或烷基，所述方法包括使下式的酸衍生物：其中X是N 或CH; Y是一个适当的离开组; Z是卤素，OR 1，NHR 1或SR 1; 并且R 1是低级烷基; 并且脒衍生物是其中R是芳基，杂芳基或烷基。

    Quinazoline derivatives as medicaments
    8.
    发明申请
    Quinazoline derivatives as medicaments 有权
    喹唑啉衍生物作为药物

    公开(公告)号：US20050096333A1

    公开(公告)日：2005-05-05

    申请号：US10957183

    申请日：2004-09-30

    Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

    Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

    IPC: A61K20060101 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  C07D471/04 ,  C07D475/10 ,  C07D487/04

    CPC classification number: C07D471/04 ,  C07D475/10 ,  C07D487/04

    Abstract: Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ═O, ═N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.

    Abstract translation: 喹唑啉衍生物具有下式：或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8各自为N或CH，其中一个或多个 两个Z 5，Z 6，Z 7和Z 8是N，并且其中两个相邻的Z位置不能是 N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1个基团可以连接形成5-6个成员的脂肪族杂环; 其中R 2独立地是R 1，R 2，R 2卤素，OR-卤素，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12 - 烯基，C

    Quinazoline derivatives as medicaments
    9.
    发明授权
    Quinazoline derivatives as medicaments 有权
    喹唑啉衍生物作为药物

    公开(公告)号：US06277989B1

    公开(公告)日：2001-08-21

    申请号：US09525034

    申请日：2000-03-14

    Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    IPC: C07D23942

    CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    Abstract: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

    Abstract translation: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。

    Quinazoline derivatives as inhibitors of P-38 &agr;
    10.
    发明授权
    Quinazoline derivatives as inhibitors of P-38 &agr; 有权
    喹唑啉衍生物作为P-38α的抑制剂

    公开(公告)号：US06184226B2

    公开(公告)日：2001-02-06

    申请号：US09141916

    申请日：1998-08-28

    Applicant: Sarvajit Chakravarty ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    Inventor： Sarvajit Chakravarty ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    IPC: A01N5500

    CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    Abstract: The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substituents which substituents are selected from the group consisting of alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C) which are useful as antiinflammatories and in treating cardiac disorders.

    Abstract translation: 本发明描述了下式的化合物及其药学上可接受的盐及其药学上可接受的盐，其中R2各自独立地为非干扰性取代基; m为0-4的整数; Z为CH或N; R 1为H，烷基（1-6C） （1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN等的任选取代的芳基， CF 3和NO 2，其中每个R独立地为H或低级烷基（1-4C）; n为0,1或2; Ar为苯基，吡啶基，吲哚基或嘧啶基，各自任选被选自以下的基团取代： 任选取代的烷基（1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，SO2NR2，CN，CF3和NO2，其中每个R独立地为H或低级烷基 （1-4C）; 和R 3是支链或环状烷基（5-7C），或是任选被1-2个取代基取代的苯基，所述取代基选自烷基（1-6C），卤素，OR，NR2，SR，-OOCR， -NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN，CF3和NO2，其中每个R独立地为H或可用作抗炎剂和治疗心脏疾病的低级烷基（1-4C）。

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